Potent
and selective non-competitive mGlu5 antagonist that displays inverse
agonist properties; blocks mGlu5 constitutive activity in vitro (IC50
= 87 nM). Acts at an allosteric modulatory site shared with MPEP and binds the
mGlu5 receptor with Kd values of 54 and 31 nM for rat and
human receptors respectively. Displays anxiolytic activity following oral
administration in vivo.
Porter et al (2005) Description of a clinically
validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49
(Suppl. 1) 267. Porteret al
(2005) Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a
potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse
agonist activity. J.Pharmacol.Exp.Ther. 315 711.